This is a phase 1/2, open-label, first-in-human study designed to evaluate the safety, tolerability,
pharmacokinetics, and overall response rate of LOXO-305 in patients with previously treated
CLL/SLL, Waldenström’s macroglobulinemia (WM)/mantle cell lymphoma (MCL)/marginal zone lymphoma (MZL),
follicular lymphoma, diffuse large B-cell lymphoma, or other B-cell NHL who have failed or are intolerant to the standard of care.

About BTK

BTK, one of the 5 members of the Tec family of non-receptor tyrosine kinases, plays a critical role in oncogenic signaling.1
BTK is a cytoplasmic tyrosine kinase, and its activation results in downstream signaling that controls nuclear factor-κB,
which is essential for normal B-cell function.1,2 BTK plays a critical role in the proliferation and survival of leukemic B-cells and is implicated
in various B-cell malignancies including CLL, MZL, MCL, and WM.1,3

About BTK inhibition

Covalent BTK inhibitors, like Imbruvica® (ibrutinib) and Calquence® (acalabrutinib), are currently approved for treating patients with B-cell malignancies.4,5
Both agents potently inhibit BTK by forming an irreversible, covalent bond with the cysteine residue at position 481 (C481) in the adenosine triphosphate pocket of the BTK.6-8
Their long-term efficacy can be limited by acquired resistance and intolerance to therapy.8,9

For additional information about the LOXO-305 clinical trial, please refer to clinicaltrials.gov.

Loxo Oncology is committed to helping patients who have not responded to available therapies and may benefit from its investigational therapies. Loxo Oncology's Policy for Access to Investigational Agents describes the principles and government regulations that the company will follow when considering a request.